Cation dependence of opioid receptor binding supports theory on membrane-mediated receptor selectivity |
| |
Authors: | D F Sargent J W Bean H W Kosterlitz R Schwyzer |
| |
Institution: | Department of Molecular Biology and Biophysics, Swiss Federal Institute of Technology, Zürich. |
| |
Abstract: | A quantitative analysis of the binding of dynorphin A-(1-9)-nonapeptide to the opioid Kappa-receptors of the guinea pig cerebellum Paterson et al. (1986) Proc. Natl. Acad. Sci. U.S.A. 83, 6216-6220] shows that changes in electrostatic surface accumulation of the ligand fully account for the observed suppression of binding by a series of univalent and divalent salts. Binding to mu- and delta-receptors, on the other hand, is subject to additional ion-specific effects. These observations support the membrane locations for the receptor sites proposed by the "membrane compartments" theory for opioid receptor selection. |
| |
Keywords: | |
|
|